Process for making histamine antagonists

Details Process for making histamine antagonists Process for making histamine antagonists

C - Chemistry, Metallurgy

07

D

260/255

C07D 239/47 (2006.01) C07D 403/02 (2006.01)

Patent

CA 1133481

ABSTRACT OF THE DISCLOSURE 2-Aminopyrimidones which are histamine H2-antagonists having the structure Image in which Het is a nitrogen-containing 5- or 6- membered fully unsaturated heterocyclic group, m is 0 or 1, Y is methylene, oxygen or sulphur, n is 2 or 3, Z is hydrogen or lower alkyl, A is an alkylene group or an alkylene group interrupted by oxygen or sulphur, and B is hydrogen or a methyl, cycloalkyl, heteroaryl, phenyl, naphthyl, benzodioxolyl or dihydrobenzodioxinyl group, are prepared by a process in which an amine Het-(CH2)mY(CH2)nNH2 is reacted with a 2-nitroaminopyrimidone of structure Image The new 2-nitroaminopyrimidone intermediates are prepared by reacting nitroguanidine with an oxoester RO2CCH(COZ)-A-B where R is lower alkyl.

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